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| | PROCHLORPERAZINE MALEATE Basic information |
| | PROCHLORPERAZINE MALEATE Chemical Properties |
| Melting point | 1750C | | storage temp. | 2-8°C | | solubility | Very slightly soluble in water and in ethanol (96 per cent). | | form | neat | | pka | pKa 8.1(H2O,t =24±1) (Uncertain) | | color | White | | λmax | 313nm(MeOH)(lit.) | | Merck | 14,7761 | | Stability: | Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Codes | Xn | | Risk Statements | 20/21/22 | | Safety Statements | 36 | | WGK Germany | 3 | | RTECS | SO3150000 | | HS Code | 2934302300 | | Toxicity | LD50 in mice (mg/kg): 400 s.c.; 120 i.p.; 90 i.v., 400 orally (Courvoisier) |
| | PROCHLORPERAZINE MALEATE Usage And Synthesis |
| Description | Prochlorperazine maleate (84-02-6) inhibits dynamin and clathrin-mediated endocytosis (CME) with an IC50=5.8 μM for CME.1?Increases tumor cell antigen presentation enhancing the efficacy of anti-tumor mAbs.2?A clinically useful antipsychotic agent3?with antimigraine4?and antiemetic activity5. | | Chemical Properties | Off-White Powder | | Uses | Antiemetic;Dopamine antagonist | | Uses | Antiemetic. | | Brand name | Compazine (GlaxoSmithKline). | | General Description | Prochlorperazinemaleate, 2-chloro-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazinemaleate (Compazine), is in the piperazine subgroupof the phenothiazines, characterized by high-milligramantipsychotic potency, a high prevalence of EPS, and lowsedative and autonomic effects. Prochlorperazine is more potenton a milligram basis than its alkylamino counterpart,chlorpromazine. Because of the high prevalence of EPS, however,it is used mainly for its antiemetic effect, not for its antipsychoticeffect. | | Biological Activity | D 2 receptor antagonist. Also interacts with 5-HT 3 and nAChR. Displays antipsychotic, antispasmodic, antiemetic and antinociceptive activity in vivo . | | Biochem/physiol Actions | Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic | | References | References/Citations
1) Daniel?et al.?(2015),?Phenothiazine-derived antipsychotic drugs inhibit dynamin and clathrin-mediated endocytosis; Traffic,?16?635
2) Chew?et al.?(2020),?Endocytosis Inhibition in Humans to Improve Responses to ADCC-Mediating Antibodies; Cell,?180?895
3) Hollister?et al.?(1969),?Clinical use of psychotherapeutic drugs: current status;?Clin. Pharmacol. Ther.,?10?170
4) Cook and Newberry (2018),?Emergency Department Use of Intravenous Prochlorperazine for Acute Migraine; Adv. Emerg. Nurs. J.,?40?148
5) Van den Berg?et al.?(1996),?The prophylactic antiemetic efficacy of prochlorperazine and ondansetron in nasal septal surgery: a randomized double-blind comparison; Anaesth. Intensive Care,?24?538 |
| | PROCHLORPERAZINE MALEATE Preparation Products And Raw materials |
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